Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 126, Issue -, Pages 52-60Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.09.099
Keywords
Chalcone derivatives; Replacing enone bridge; Cytotoxic activity; Cancer cell lines; Normal cell lines; Tubulin beta polymerization inhibitors
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A series of chalcone analogous compounds were designed and synthesized. Replacing/substituting the enone or ethylenic bridge of the parent chalcone with rigid heterocyclic moieties or substituted aromatic amines gave nineteen target compounds. Their cytotoxic activities were screened against both breast and liver cancer cells as well as breast and liver normal cells. Target compounds were also evaluated for their inhibition activity of tubulin beta polymerization. Target compound 2e, 3a, 3b, 3c, 4a -4d, 5a, 5b and 6 showed broad spectrum excellent anticancer activity against both MCF-7 and HepG2. Compound 4a showed the most TUBb inhibition activity. (C) 2016 Elsevier Masson SAS. All rights reserved.
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